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REFERENCE LINKING PLATFORM OF KOREA S&T JOURNALS
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Biomolecules and Therapeutics
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Journal DOI :
The Korean Society of Applied Pharmacology
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Volume & Issues
Volume 5, Issue 4 - Dec 1997
Volume 5, Issue 3 - Sep 1997
Volume 5, Issue 2 - Jun 1997
Volume 5, Issue 1 - Mar 1997
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Modulation of Ligand Binding to the GABA-benzodiazepine Receptor Complex by Gastrodia elata Blume
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 325~330
Methanol extract of G. elata inhibited the binding of [/sup 3/H]Rol5-1788, a selective benzodiazepine receptor antagonest, to benzodiazepine receptor of rat cortices. Saturation experiments followed by Scatchard analysis of the results showed that the inhibition of [sub 3/H]Ro15-1788 binding by G. dlata. appeared to be com-petitive. These competitive inhibiton of the butanol fraction was observed to be higher than the methanol extract. Methanol extract of G. efara inhibited a [sub 3/H]flunitrazepam, a selective benzodiazepine receptor agonist, binding to benzodiazepine receptor. GABA significantly enhanced the inhibition of [/sub 3/H]flunitrazepam binding by G. elata, and these "positive GABA shift" supported the strong possibility of agonestic activity to benzodiazepine receptor Butanol fraction was observed to be higher than crude extract by methanol in an agonistic activity to benzodiazepine receptor, furthermore enhanced the binding of [sub 3/H]SR95531 to GABA receptor. Butanol fraction of G. elata significantly diminished the pentylenetetrazole-induced lethality of mice. From these results, it can be concluded that substance or substances with neurochemical properties characteri- stic of a benzodiazepine receptor agonist may be important components, and contribute to the anticonvulsant property of G. elata.
Antigastritic and Antiulcer Actions of the Fraction of Taheebo
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 331~335
In a preliminary screening of plant extracts for the antigastritic and antiulcer actions in rats, the methanol extracts of Taheebo showed positive activity in HCI . ethanol-induced gastric lesion. Among the systematic fractions of hexane, chloroform, butanol and water, the most potent
fraction reduced significantly HCI . ethanol-induced gastric lesion at the oral dose of 300 mg/kg. In pylorus ligated rats chloroform and butanol fraction showed decreases in the volume of gastric secretion and acid output of which effects were stronger in chloroform fraction. Further assays with hexane butanol and
fraction disclosed that it significantly suppressed the aspirin-induced ulcer. The butanol fraction reduced significantly acetic acid induced ulcer at the dose of 400 mg/kg. The butanol and
fraction reduced the malondialdehyde level in HCI . ethanol-induced gastric lesion. In pylorus ligated rats, chloroform and butanol fraction reduced the malondialdehyde level and in aspirin-induced ulcer, chloroform fraction reduced that levle. These results might suggest that the butanol and
fraction of Taheebo had inhibitory action in gastric lesion and ulceration through inhibition of gastric acid secretion and the decrease malondialdehyde level.
Relationship between the Regulation of Blood Pressure and in vivo Noradrenergic Neural Activities in the Locus Coeruleus of Young Spontaneously Hypertensive Rats
Kim, Yun-Tai ; Lee, Jin-Hwa ; Lee, Eun-Kyung ; Lee, Chung-Jae ; Cheong, Jae-Hoon ; Jin, Chang-Bae ; Ko, Kwang-Ho ;
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 336~343
The purpose of the present study was to address whether the in vivo noradrenergic neural activities in the locus coeruleus are related to the development of hypertension. Two groups of the animals were prepared, 1) young SHR and 2) age-matched normotensive control, WKY. At the age of 6 weeks, blood pressure and the releases of NE and DOPEG from the locus coeruleus in young SHR and WKY were measured by in vivo microdialysis at two different conditions; 1) normal and 2) elevated state of blood pressure by systemically injected phenylephrine. Basal releases of NE and OOPEG from the locus coeruleus were
pg/20 min and
pg/20 min in SHR and
pg/20 min and
pg/20 min in WKY The basal release of NE of SHR was significantly greater than that of WKY. Phenylephrine treatment caused elevation of blood pressure in both SHR and WKY in dose-dependent manner. Following phenylephrine injection, the releases of NE and DOPEG from the locus coeruleus of SHR were significantly decreased, whereas there was no significant changes of NE in WKY. The results from the present study suggests that the noradrenergic nervous system in the locus coeruleus may contribute as one of the triggering factors for the expression of hypertension in young SHR.
Production and Characterization of a Monoclonal Antibody against Human
Kang, Suk-Jo ; Shin, Chan-Young ; Song, Mi-Ryoung ; Lee, Chung-Jae ; Cheong, Jae-Hoon ; Lee, Sang-Bong ; Ko, Kwang-Ho ;
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 344~350
The purpose of the present study was to produce and characterize a monoclonal antibody against human
-adrenergic receptor. Male BALB/c mice were immunized with glutathione S-transferase (GST) fusion protein of the C-terminal portion of the human
-adrenergic receptor which was expressed in E.Coli. The immunized splenocytes were fused with myeloma SP2/0-Agl4 cells. The resulting hybridomas were screened for the production of a monoclonal antibody which can recognize human
-adrenergic receptor, and then subcloned by limiting dilution. The resulting monoclonal antibody was named as mAb
CO2. The mono-clonal antibody
CO2 was determined as IgM subtype and then purified by anti-mouse IgM-agarose affinity chromatography. The results of ELISA, Western blot, and immunocytochemistry showed that mAb
CO2 recognized human
-adrenergic receptor in the
-adrenergic receptor-GST fusion protein and human spider-moid carcinoma cell line A431 with highly specific immunoreactivity, The monoclonal antibody
CO2 may provide useful tools for the study of the
-adrenergic receptor of human and other species including rats.
Effect of Renal Denervation on Diuretic Action of UK 14,304,
-Adrenergic Agonist, in Dog
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 351~356
This study was performed in order to investigate the effect of renal denervation on diuretic action of UK 14, 304,
-Adrenergic Agonist, administered into the vein and the carotid artery in dog. The diuretic action of UK 14, 304 administered into the vein or the carotid artery was reversed to the antidiuretic action by renal denervation, this time, the decrease of N
excretion amounts in urine (
) and the increase of N
reabsorption rates in renal tubule (
) were exhibited. This results suggest that central diuretic action of UK 14, 304 is mediated by renal nerves and the antidiuretic action of UK 14, 304 in denervation kidney is caused by the increase of N
reabsorption rates (
) in renal tubules in dog.n dog.
Skin Permention of Ketoprofen from Lotion
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 357~363
The effects of formulation variables of topical lotion on the skin permeation of ketoprofen were evaluated using excised rat skins. The formulation variables were the amounts of poloxamer 407, drug and ethanol, and penetration enhancers. The Keshary-Chien diffusion cells were used for the diffusion study. The flux of ketoprofen linearly decreased as the concentration of poloxamer increased from 5% to 15% in the preparation, and linearly increased as the amount of drug increased. Penetration enhancers such as fatty acids and fatty alcohols showed markedly enhancing effects at the level of 5%. Among them, the highest flux was shown in linolenic acid. From these results, optimum formula containing 3% ketoprofen, 5% poloxamer 407, 40% ethanol and 5% linolenic acid having the flux of 537.6
/hr were noted.
Influence of Age and Fasting on the Anti-hyperglycemic Effect of Onion in Normal and Diabetic rat
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 364~368
Onion (Allium cepa Linn) has been reported to have hypoglycemic activity in human and several animal models. In the present study, we performed intraperitoneal glucose tolerance test (IPGTT) in young (1.5mo) and aged (5 mo) rats treated with onion in order to determine whether aging can influence on the anti-hy-perglycemic effect of onion. In addition, we investigated the hypoglycemic effect of onion in streptozotocin- induced diabetic rats treated with aqueous extracts of onion (500 mg/kg, i.p., daily) for 4 weeks. Blood glucose level was determined in fasted and fed rats by using a glucometer (Johnson & Johnson). In glucose tolerance test, blood glucose level was maximally increased 15 min after glucose load (2 g/kg, i.p.), and recovered to the basal level 3 hr after glucose challenge in young and old rats. The maximum blood glucose levels of young and aged rat were 184
7.49 and 225.2
12.55 mg/dl, respectively. A single i.p. injection of aqueous extract of onion (1 g/kg) 30 min before glucose challenge significantly decreased blood glucose levels at 15, 30, 60, 90 min after glucose load in aged rats, while the administration of onion did not show any significant effect in young rats. In onion-treated diabetic rats, significant hypoglycemic effect (p<0.05) was observed, and the effect was greater in fasted rats than in fed. In conclusion, these results suggest that anti-hyperlycemic effect of onion can be changed by age and fasting.
General Pharmacology of SB-31
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 369~375
General pharmacological effects of SB-31
, the extracts of Pulsatilla koreana, were investigated in mice, rats and guinea-pigs. Intravenous injection of SB-31 (3 and 6 ml/kg) produced almost no effect on central nervous system no effects on the general symptom and behaviors of mice, spontaneous locomotor activity, pentobarbital- induced sleeping time , rotared performance , electroshock and pentylenetertrazole -induced seizures, acetic acid-induced writhing and normal body temperature in mice. SB-31 showed little effects on the spontaneous movement of the isolated ileum and contraction induced by agonists in isolated ileum, suggesting no influence on autonomic nervous system. Administration of SB-31 also did not show any effect on blood pressure in conscious rats. However, a slight decrease in heart rate was observed at high doses (6 and 10 ml/kg) of SB-31 in conscious rats. Similarly, a slight increase in respiratory rate was observed at 6 m1/kg of SB-31 in anesthetized rats. SB-31 did not produce any effect at the dose of 3 ml/kg, but showed a tendency to increase the urinary volume at 6 ml/kg, and produced a decrease in urinary excretions of N
at 6 ml/kg. However, transport capacity within the gastrointestinal tract and the secretion of the gastric juice were not influenced by 6 ml/kg of SB-31. In conclusion, these results suggest that SB-31 did not pro-duce any acute effects on the central nervous system, autonomic nervous system, respiratory and circulatory systems, digestive system and kidney function at the dose of below 3 ml/kg.ml/kg.
Effect of CJ-50001 (rG-CSF) on the Recovery of the Neutrophil Numbers in the Mice with Bone Marrow Transplantation BMT)
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 376~379
The peripheral neutrophil recovery test was conducted to determine the efficacy of CJ-50001, a drug developed in Cheil Jedang R&D center as a recombinant granulocyte-colony stimulating factor (rG-CSF). Grasin was used as control drug. CJ-50001 and Gratin were subcutaneously administered to
-ray irradiated mice for 21 days at a dose of 10
g/kg after bone marrow transplantation and the recovery of neutrophil number was examined on the days of 9, 13, 17, and 21 after the drug administration. It was observed that the peripheral neutrophil number of the vehicle control group was recovered to the normal level on the day of 13 after the transplantation whereas the group administered with CJ-50001 and Grasin respectively, showed the normal level of peripheral neutrophil number on 9th day after the bone marrow transplantation. The number of peripheral neutrophils reached the highest level on the 21 st day of drug administration, and was recovered to the normal level on the 4th day after ceasing of the drug administration (on the 25th day of the transplantation). Thus, it was presumed that CJ-50001 showed efficacy similar to Grasin on the peripheral neutrophil recovery after bone marrow transplantation.
The Effect of a Single Administration of rG-CSF on the Peripheral Neutrophil Levels and Its Dose Responsiveness in Normal ICR mice and SD rats
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 380~383
CJ-50001 is a recombinant granulocyte-colony stimulating factor (rG-CSF) developed by Cheil Jedang R&D Center. The effects of CJ-50001 on the increase of peripheral neutrophil count following intravenous and subcutaneous single administration at a dose of 20
g/kg in normal ICR mice and SD rats, respectively, were compared with those of Grasin, a control drug. Both CJ-50001 and Grasin significantly increased the peripheral neutrophil number in four treatment groups and the maximum number of neutrophil was achieved at 12 to 18 h in rats and mice, respectively. The dose dependency test was studied for CJ-50001 only in normal mice by intravenous or subcutaneous administration. When administered i.v or s.c at the various doses in normal mice, CJ-50001 significantly increased the neutrophil number over the dose of 160 ng/kg, compared with the vehicle control group. From these results, it was concluded that CJ-50001 showed efficacy similar to Grasin in the peripheral neutrophil count increase.
Therapeutic Effect of CJ-50(101 (rG-CSF) on Neutropenia Caused by Anticancer Agents in Mice
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 384~389
Neutropenia is a major dose-limiting side effect of cancer chemotherapy. The therapeutic effects of CJ-50001 were examined on neutropenia caused by anticancer agents. Neutropenia was induced by cyclophosphomide (130 mg/kg), doxorubicin (4.5 mg/kg), and vincristine (1 mg/kg) in normal ICR mice and by cyclophosphamide (200 mg/kg) in CT26 adenocarcinoma bearing BALB/C mice. After the subcutaneous injection of anticancer agents, we administered subcutaneously recombinant human granulocyte-colonystimulating factor (100
g/kg/day) to mice in order to stimulate neutrophil production. In normal and tumor-bearing mice, neutrophil production efficacy of CJ-50001 (rG-CSF) was similar to that of Grasin. These results suggest that CJ-50001 could be effective in its clinical use for neutropenia treatment.
Pharmacological Actions of New Woohwangchungsimwon Liquid on Cardiovascular System
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 390~401
In order to investigate the pharmacological properties of New Woohwangchungsimwon Liquid (NCL), effects of Woohwangchungsimwon Liquid (CL) and NCL were compared. In isolated rat aorta, NCL and CL showed the relaxation of blood vessels in maximum contractile response to phenylephrine (10
M) without regard to intact endothelium or denuded rings of the rat aorta. Furthermore, the presences of the inhibitor of NO synthase and guanylate cyclase did not affect the relaxation of NCL and CL. NCL and CL inhibited the vascular contractions induced by acetylcholine, prostaglandin endoperoxide or peroxide in a dose-dependent manner. In conscious spontaneously hypertensive rats (SHRs), NCL and CL significantly decreased heart rate. NCL and CL, at high doses, had a negative inotropic effect that was a decrease of LVDP and (-dp/dt)/(+dp/dt) in the isolated perfused rat hearts, and also decreased the contractile force and heart rate in the isolated rat right atria. In excised guinea-pig papillary muscle, NCL and CL had no effects on parameters of action potential at low doses, whereas inhibited the cardiac contractility at high doses. These results suggested that NCL and CL have weak cardiovascular effects with relaxation of blood vessels and decrease of heart rate, and that this effect is no significant differences between two preparations.
Pharmacological Actions of New Woohwangchungsimwon Liquid on Cerebral Ischemia and Central Nervous System
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 402~411
ln order to investigate pharmacological properties of New Woohwangchungsimwon Liquid (NCL) and Woohwangchungsimwon Liquid (CL), effects of NCL and CL on cerebral ischemia and central nervous system were compared. Cerebral ischemia insult was performed using unilateral carotid artery occlusion in Mongolian gerbils. The histological observations showed a preventive effect of NCL and CL treatments with ischemia-induced brain damage. The ATP in brain tissue was decreased in vehicle-treated ischemic gerbils. This decrease was prevented by CL treatment. In contrast to what was seen with ATP, the lactate and lipid peroxide were both elevated in vehicle-treated ischemic gerbils. This elevation was inhibited by NCL and CL treatments. While NCL and CL had no effects on the hexobarbital-induced sleeping time, they prevented the seizures induced by electric shock and pentetrazol. NCL and CL showed sedative effect in rotarod and spontaneous activity test. Respiration rate and depth were increased at the high dose of NCL and CL. Furthermore, NCL and CL showed anti-stress effect. Our findings suggest that the pharmacological profile of NCL on cerebral ischemia and central nervous system are similar to that of CL.
General Pharmacology of AG 60, a New Anticancer Drug
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 412~418
General pharmacological properties of AG 60 (mixture of acriflavine and guanosine (1:1, w/w)), which has anticancer effect, following intramuscular administration were examined in terms of effects on central nervous system, gastrointestinal system, cardiovascular system, respiratory system and autonomic nervous system in mice, rats, guinea-pigs and rabbits. AG 60 at the dose of 15 mgtg had no influences on pentobarbital sleeping time, spontaneous motor activity, chemoshock produced by pentylenetetrazole solution, writhing syndromes induced by 0.8% acetic acid solution, and motor coordination of mice. However, AG 60 at the dose of 7.5 and 15 mg/kg caused significant decrease of normal body temperature 1 and/or 2 h after the administration. No influence on body temperature was observed at 3.75 mg/kg in mice. Gastric secretion of rat and intestinal motility of mice were not influenced by the dose of 15 mg/kg. In terms of autonomic nervous system, AG 60 did not show direct effect and inhibitory or augmentative action of histamine- or acetylcholine-induced contractions at the concentration of 5 mg/L in the isolated ileum of guinea-pig. The administration of 15 mg/kg of AG 60 did not affect mean arterial blood pressure and heart rate in rat. AG 60 (15 mg/kg) given to anesthetized rabbits showed no effect on respiratory rate.
Pharmacokinetics and Tissue Distribution of a New Fluoroquinolone Containing C7-Bicyclic Structure in Rats
Biomolecules and Therapeutics, volume 5, issue 4, 1997, Pages 419~425
The pharmacokinetics of DWP20364 (1-cyclopropyl -5-amino-6,8-difluoro-7-(2,7-diazabiclo [3,3,0] oct-4-ene-7-yl)-1,4-dihydro-4-oxoquinoline-3-carboxylic acid), a novel fluoroquinolone containing C7-bicyc-talc structure, were compared with those of ciprofloxacin (CPFX) after single intravenous (i.v.) and oral (p.o.) administration to rats using microbiological assay (bioassay). After i.v. administration to rats, the plasma concentrations of the two drugs declined biexponentially. The terminal half-lives (t
/) of DWP20364 were 110
13.2 min and 117
3.09 min after i.v. and p.o. administration, respectively, and they were significantly higher than those of CPFX (45.5
9.52 min and 48.3
12.1 min, respectively). Similar results were also obtained from plasma concentrations and area under the plasma concentration-time curves. The total body clearance of DWP20364, 7.82
0.37 ml/min/kg was significantly slower than that of CPFX, 27.3
11.1 m1/ min/kg. Above data suggested that the antimicrobial activity of DWP20364 could be longer than that of CPFX. The urinary recovery after i.v. and p.o. administration of DWP20364 was significantly lower than those of CPFX suggesting that the effect of DWP20364 on urinary tract infection could be lower than that of CPFX. The serum protein binding values of DWP20364 at 2
g/ml were apparently 91.5~93.1% in rats and human. DWP20364 was distributed by the order of liver, lung, kidney, sf)leon, heart, muscle and brain collected at 30 min after orally administered.